IMPROVED PREPARING METHOD OF (S)-OMEPRAZOLE FROM OMEPRAZOLE RACEMATE USING OPTICAL RESOLUTION AGENT

摘要

A method for preparing (S)-omeprazole from omeprazole racemate is provided to improve optical purity of (S)-omeprazole by using an optical resolution agent, so that the high optical purity of (S)-omeprazole is useful as a raw material of medicines. A method for preparing (S)-omeprazole from omeprazole racemate comprises the steps of: (a) reacting omeprazole racemate, optically active diethyl-D-tartrate and titanium compound in alcohol to prepare omeprazole racemate complex; (b) reacting the omeprazole racemate complex with 1.5-3.0 mole equivalent of (S)-(+)-mandelic acid as an optical resolution agent to prepare optically active omeprazole racemate complex; and (c) reacting the optically active omeprazole racemate complex with base solution to prepare (S)-omeprazole free base, and optionally reacting the (S)-omeprazole free base with metal salt to prepare metal salt or metal salt hydrate of (S)-omeprazole with optical purity of 99.0%ee or more. The omeprazole racemate is omeprazole racemate free base or metal salts thereof or metal salts hydrate thereof.